Levonorgestrel Microneedle Array Patch for Sustained Release Contraception: Formulation, Optimization and In Vivo Characterization

Rajput, Amarjitsing; Osmani, Riyaz Ali M.; Khire, Achyut; Jaiswal, Sanket; Banerjee, Rinti

doi:10.3390/molecules27072349

Cited by 13 publications

(6 citation statements)

References 52 publications

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“…A microneedle patch consists of a thin adhesive paper with microneedles made of biodegradable material. LNG is embedded in the microneedles with an average length and base diameter of 900 and 300 µ m, respectively [141]. Once applied, the adhesive paper detaches and leaves the microneedles in the top skin layer, approximately 1 mm deep.…”

Section: Female Hormonal Methodsmentioning

confidence: 99%

Reversible female contraceptives: historical, current, and future perspectives

Barton,

Erickson,

Allred

et al. 2023

Biology of Reproduction

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Contraception is a practice with extensive and complicated social and scientific histories. From cycle tracking, to the very first prescription contraceptive pill, to now having over-the-counter contraceptives on demand, family planning is an aspect of healthcare that has undergone and will continue to undergo several transformations through time. This review provides a comprehensive overview of current reversible hormonal and non-hormonal birth control methods as well as their mechanism of action, safety, and effectiveness specifically for individuals who can become pregnant. Additionally, we discuss the latest Food and Drug Administration (FDA)-approved hormonal method containing estetrol and drospirenone that has not yet been used worldwide as well as the first FDA-approved hormonal over-the-counter progestin-only pills. We also review available data on novel hormonal delivery through microchip, microneedle, and the latest FDA-approved non-hormonal methods such as vaginal pH regulators. Finally, this review will assist in advancing female contraceptive method development by underlining constructive directions for future pursuits. Information was gathered from the NCBI and Google Scholars databases using English and included publications from 1900 to present. Search terms included contraceptive names as well as efficacy, safety, and mechanism of action. In summary, we suggest that investigators consider the side effects and acceptability together with the efficacy of contraceptive candidate towards their development.

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Section: Female Hormonal Methodsmentioning

confidence: 99%

Reversible female contraceptives: historical, current, and future perspectives

Barton,

Erickson,

Allred

et al. 2023

Biology of Reproduction

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“…The chromatographic data were recorded, analyzed, and saved using Chromatography Data System software (ChromNAV 2.0, Jasco, Tokyo, Japan) [ 34 ]. After drug amount estimation, the EE and DL was calculated using the following formulas [ 35 , 36 ]:

…”

Section: Methodsmentioning

confidence: 99%

Formulation, Characterization, and Evaluation of Eudragit-Coated Saxagliptin Nanoparticles Using 3 Factorial Design Modules

et al. 2022

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Background and Introduction: Saxagliptin is a hypoglycemic drug that acts as a dipeptidyl peptidase-4 (DPP-4) inhibitor and is preferably used in the treatment of Type 2 Diabetes Mellitus (T2DM). It is safe and tolerable; however, the major disadvantage associated with it is its low bioavailability. Aim: The present research aimed to enhance the bioavailability of the drug by enteric coating with a polymer that controls the rate of drug delivery, and it was prepared as Solid Lipid Nanoparticles (SLNs). Methodology: In the current study, various SLN formulations were developed using a central composite design (CCD) module using Design Expert-11 software. A modified solvent injection technique was used to prepare Saxagliptin nanoparticles coated with Eudragit RS100. The CCD was used to determine the independent variables and their effect on dependent variables at varied levels. Evaluation studies such as particle size analysis, Zeta potential, polydispersity index (PDI), drug loading, entrapment efficiency, in-vitro drug release studies, and in vivo pharmacokinetic studies were performed for the optimized SLN formulation. The reversed-phase HPLC method was developed and validated for the estimation of the pharmacokinetic parameters of the pure drug and prepared SLNs. Results: The effect of independent variables (A1: amount of lipid, A2: amount of polymer, A3: surfactant concentration, and A4: homogenization speed) on dependent variables (R1: particle size, and R2: entrapment efficiency) was established in great detail. Observed responses of the prepared and optimized Saxagliptin SLN were close to the predicted values by the CCD. The prepared SLNs depicted particle sizes in the range of 212–442 nm. The particle size analysis results showed that an increase in the lipid concentration led to an increase in particle size. The developed bioanalytical method was noted to be very specific and robust. The method accuracy varied from 99.16% to 101.95% for intraday, and 96.08% to 103.12% for inter day operation at low (5 mcg/mL), moderate (10 mcg/mL), and higher (15 mcg/mL) drug concentrations. The observed Zeta potential values for the prepared SLNs were in the range of −41.09 ± 0.11 to 30.86 ± 0.63 mV suggesting quite good stability of the SLNs without any aggregation. Moreover, the polydispersity indices were in the range of 0.26 ± 0.051 to 0.45 ± 0.017, indicative of uniformity of sizes among the prepared SLNs. In vivo study outcomes proved that Saxagliptin oral bioavailability significantly enhanced in male Albino Wistar Rats via SLN formulation and Eudragit RS100 coating approach. Conclusions: The developed and optimized Saxagliptin SLNs revealed enhanced Saxagliptin bioavailability in comparison to the native drug. Thus, this formulation strategy can be of great importance and can be implied as a promising approach to enhance the Saxagliptin bioavailability for facilitated T2DM therapy.

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“…Among the different NPs, LVs stand out by their biocompatibility and versatility, as they allow modifications with surfactants (transfersomes) or ethanol (ethosomes) to improve their skin delivery ability. Rajput et al prepared levonorgestrel (LVN) liposome (LPs) loaded into PVA-based MAPS (LVN-LPs@MAPs) for contraception purposes (Rajput et al, 2022). In an in vivo study with rats, LVN@MAPs reached therapeutic concentrations in 10 days, whereas LVN-LPs@MAPs needed 2 days less to reach the same levels (200 μg/ml) and maintained a LVN concentration above the human therapeutic level for more than 1 month, showing that they are useful as longacting contraceptives.…”

Section: Lipid-based Nanoparticlesmentioning

confidence: 99%

Microneedle‐assisted transdermal delivery of nanoparticles: Recent insights and prospects

Guillot

Martínez-Navarrete

Zinchuk-Mironova

et al. 2023

WIREs Nanomed Nanobiotechnol

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Transdermal delivery of drugs offers an interesting alternative for the administration of molecules that present certain troubles when delivered by the oral route. It can produce systemic effects or perform a local action when the formulation exerts an optimal controlled drug release or a targeted delivery to the specific cell type or site. It also avoids several inconveniences of the oral administration such as the hepatic first pass effect, gastric pH-induced hydrolysis, drug malabsorption because of certain diseases or surgeries, and unpleasant organoleptic properties. Nanomedicine and microneedle array patches (MAPs) are two of the trendiest delivery systems applied to transdermal research nowadays. However, the skin is a protective barrier and nanoparticles (NPs) cannot pass through the intact stratum corneum. The association of NPs and MAPs (NPs@MAPs) work synergistically, since MAPs assist NPs to bypass the outer skin layers, and NPs contribute to the system providing controlled drug release and targeted delivery. Vaccination and tailored therapies have been proposed as fields where both NPs and MAPs have great potential due to inherent characteristics. MAPs conception and easy use could allow selfadministration and therefore facilitate mass vaccination campaigns in undeveloped areas with weak healthcare services. Additionally, nanomedicine is being explored as a platform to personalize therapies in such an important field as oncology. In this work we show recent insights that prove the benefits of NPs@MAPs association and analyze the prospects and the discrete interest of the industry in NPs@MAPs, evaluating different limiting steps that restricts NPs@MAPs translation to the clinical practice.

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Levonorgestrel Microneedle Array Patch for Sustained Release Contraception: Formulation, Optimization and In Vivo Characterization

Cited by 13 publications

References 52 publications

Reversible female contraceptives: historical, current, and future perspectives

Reversible female contraceptives: historical, current, and future perspectives

Formulation, Characterization, and Evaluation of Eudragit-Coated Saxagliptin Nanoparticles Using 3 Factorial Design Modules

Microneedle‐assisted transdermal delivery of nanoparticles: Recent insights and prospects

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